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PA8629901A1 - Sintesis regioespecifica de derivados de 42-ester de rapamicina - Google Patents

Sintesis regioespecifica de derivados de 42-ester de rapamicina

Info

Publication number
PA8629901A1
PA8629901A1 PA20058629901A PA8629901A PA8629901A1 PA 8629901 A1 PA8629901 A1 PA 8629901A1 PA 20058629901 A PA20058629901 A PA 20058629901A PA 8629901 A PA8629901 A PA 8629901A PA 8629901 A1 PA8629901 A1 PA 8629901A1
Authority
PA
Panama
Prior art keywords
rapamycin
synthesis
regespecific
ester derivatives
derivatives
Prior art date
Application number
PA20058629901A
Other languages
English (en)
Inventor
Jianxin Gu
Ping Cai
Mark E Ruppen
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34965235&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PA8629901(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of PA8629901A1 publication Critical patent/PA8629901A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
    • C12N9/18—Carboxylic ester hydrolases (3.1.1)
    • C12N9/20—Triglyceride splitting, e.g. by means of lipase
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
    • C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

SE DESCRIBE UN METODO PARA LA SINTESIS REGIOESPECIFICA DE DERIVADOS 42-ESTER DE RAPAMICINA. EL METODO INVOLUCRA LA ACILACION CATALIZADA POR LIPASA DE 42-HIDROXI RAPAMICINA CON UN DONADOR DE ACILO TAL COMO UN VINILESTER, UN ISOPROPENILESTER O UN ANHIDRIDO EN UN SOLVENTE ORGANICO ADECUADO
PA20058629901A 2004-04-14 2005-04-13 Sintesis regioespecifica de derivados de 42-ester de rapamicina PA8629901A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US56192604P 2004-04-14 2004-04-14

Publications (1)

Publication Number Publication Date
PA8629901A1 true PA8629901A1 (es) 2006-06-02

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
PA20058629901A PA8629901A1 (es) 2004-04-14 2005-04-13 Sintesis regioespecifica de derivados de 42-ester de rapamicina

Country Status (23)

Country Link
US (1) US7268144B2 (es)
EP (1) EP1737869A1 (es)
JP (1) JP4224115B2 (es)
KR (1) KR20070015544A (es)
CN (1) CN1942476A (es)
AR (1) AR049019A1 (es)
AU (1) AU2005238431A1 (es)
BR (1) BRPI0509852A (es)
CA (1) CA2562952A1 (es)
CL (1) CL2008000507A1 (es)
CR (1) CR8646A (es)
EC (1) ECSP066927A (es)
GT (1) GT200500085A (es)
IL (1) IL178315A0 (es)
MX (1) MXPA06011881A (es)
NO (1) NO20065090L (es)
PA (1) PA8629901A1 (es)
PE (1) PE20060253A1 (es)
RU (1) RU2387657C2 (es)
SG (1) SG152234A1 (es)
TW (1) TW200536542A (es)
UA (1) UA87492C2 (es)
WO (1) WO2005105811A1 (es)

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SI1553940T1 (sl) 2002-07-30 2008-08-31 Wyeth Corp Parenteralne farmacevtske oblike, ki vsebujejo rapamicin-hidroksiester
BRPI0509810A (pt) * 2004-04-14 2007-09-18 Wyeth Corp método para a sìntese regioespecìfica de um 42-hemiéster de rapamicina ou um 32-hemiéster de fk-506 com um ácido dicarboxìlico, 42-hemiéster de rapamicina regioespecìfica, anticorpo de rapamicina, produto, e, 32-hemiéster de fk506 regioespecìfico
CA2562164A1 (en) * 2004-04-27 2005-11-10 Wyeth Labeling of rapamycin using rapamycin-specific methylases
AU2005292647A1 (en) * 2004-08-10 2006-04-13 Wyeth CCI-779 derivatives and methods of making same
CN101115759A (zh) 2005-02-09 2008-01-30 惠氏公司 Cci-779多晶形物及其应用
WO2007056175A2 (en) * 2005-11-04 2007-05-18 Wyeth 41-methoxy isotope labeled rapamycin 42-ester
EP1957964A2 (en) * 2005-12-07 2008-08-20 Wyeth Pharmaceuticals Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry
RU2008120670A (ru) * 2005-12-07 2010-01-20 Вайет (Us) Масштабируемый способ получения 42-сложного эфира рапамицина из 42-сложного эфира рапамицина бороната
AR058282A1 (es) * 2005-12-07 2008-01-30 Wyeth Corp Forma cristalina purificada de cci-779, un proceso para la preparacion del mismo, un metodo para monitorear la cristalizacion del cci-779, un kit y una composicion farmaceutica que lo comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
KR20080106225A (ko) * 2006-03-07 2008-12-04 와이어쓰 마크롤라이드 면역억제제의 수용성 폴리에틸렌 글리콜 콘쥬게이트를 제조하는 방법
US20080175887A1 (en) 2006-11-20 2008-07-24 Lixiao Wang Treatment of Asthma and Chronic Obstructive Pulmonary Disease With Anti-proliferate and Anti-inflammatory Drugs
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414526B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US20080276935A1 (en) 2006-11-20 2008-11-13 Lixiao Wang Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8414910B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
TW200845960A (en) * 2007-04-05 2008-12-01 Wyeth Corp Wortmannin-rapalog conjugate and uses thereof
US20090253733A1 (en) * 2008-04-02 2009-10-08 Biointeractions, Ltd. Rapamycin carbonate esters
US20110098241A1 (en) * 2008-04-14 2011-04-28 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
WO2010024898A2 (en) 2008-08-29 2010-03-04 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
CN101676291B (zh) * 2008-09-18 2012-05-09 上海海和药物研究开发有限公司 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途
CA2937492C (en) 2008-11-11 2019-08-13 The Board Of Regents Of The University Of Texas System Inhibition of mammalian target of rapamycin
IT1394309B1 (it) 2009-05-22 2012-06-06 Poli Ind Chimica Spa Nuovo approccio chimico-enzimatico alla sintesi del pimecrolimus
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
BR112013025085A2 (pt) * 2011-04-01 2016-07-19 Sandoz Ag processo para a acilação de rapamicina e processo para sintetizar tensirolimo
US10751450B2 (en) 2012-06-08 2020-08-25 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
DK2859001T3 (da) * 2012-06-08 2016-05-30 Biotronik Ag Rapamycin 40-o-cyklisk kulbrinteestere, sammensætninger og fremgangsmåder
US20160030401A1 (en) 2013-03-13 2016-02-04 The Board Of Regents Of The University Of Texas System Use of mtor inhibitors for prevention of intestinal polyp growth and cancer
SG10201707632PA (en) * 2013-03-15 2017-11-29 Biosensors Int Group Ltd Purification of rapamycin derivatives
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
DK3089737T3 (da) 2013-12-31 2021-12-13 Rapamycin Holdings Llc Orale rapamycin-nanopartikelpræparater og anvendelse.
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Also Published As

Publication number Publication date
CN1942476A (zh) 2007-04-04
GT200500085A (es) 2005-11-03
SG152234A1 (en) 2009-05-29
CL2008000507A1 (es) 2008-07-04
WO2005105811A1 (en) 2005-11-10
US20050234234A1 (en) 2005-10-20
CR8646A (es) 2007-08-28
RU2006134014A (ru) 2008-05-20
ECSP066927A (es) 2006-12-20
JP2007532134A (ja) 2007-11-15
US7268144B2 (en) 2007-09-11
AR049019A1 (es) 2006-06-21
CA2562952A1 (en) 2005-11-10
MXPA06011881A (es) 2006-12-14
NO20065090L (no) 2006-11-13
TW200536542A (en) 2005-11-16
KR20070015544A (ko) 2007-02-05
EP1737869A1 (en) 2007-01-03
IL178315A0 (en) 2007-02-11
PE20060253A1 (es) 2006-03-30
AU2005238431A1 (en) 2005-11-10
BRPI0509852A (pt) 2007-10-23
RU2387657C2 (ru) 2010-04-27
UA87492C2 (en) 2009-07-27
JP4224115B2 (ja) 2009-02-12

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